US8153818B2ActiveUtilityPatentIndex 61
Triazolyl phenyl benzenesulfonamides

Assignee: CHARVAT TREVOR TPriority: Jul 14, 2006Filed: Apr 2, 2010Granted: Apr 10, 2012
Est. expiryJul 14, 2026(expired)· nominal 20-yr term from priority
Inventors:CHARVAT TREVOR T HU CHENG MELIKIAN ANITA NOVACK AARON PENNELL ANDREW M K PUNNA SREENIVAS SULLIVAN EDWARD J TAN XUEFEI THOMAS WILLIAM D UNGASHE SOLOMON ZENG YIBIN
A61P 9/10A61P 37/06A61P 9/00A61P 37/00A61P 3/10A61P 3/00A61P 25/00A61P 29/00A61P 35/00A61P 3/04C07D 413/04C07D 403/04C07D 249/08A61P 1/00C07D 405/04A61P 11/00A61P 13/12C07D 401/04
PatentIndex Score
Cited by
References
Claims
Abstract

Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
Claims

exact text as granted — not AI-modified
The invention claimed is: 
     
       1. A compound of the formula (I), or a salt thereof: 
       
         
           
           
               
               
           
         
       
       where
 Ar is selected from the group consisting of substituted or unsubstituted C 6-10  aryl and substituted or unsubstituted 5- to 10-membered heteroaryl; 
 Y 4 , Y 5 , Y 6 , and Y 7  are each independently selected from the group consisting of hydrogen, halogen, —CN, —C(O)R 15 , —CO 2 R 15 , —C(O)NR 15 R 16 , —OR 15 , —OC(O)R 15 , —OC(O)NR 15 R 16 , —SR 15 , —S(O)R 15 , —S(O) 2 R 15 , —S(O) 2 NR 15 R 16 , —NO 2 , —NR 15 R 16 , —NR 15 C(O)R 16 , —NR 15 C(O)OR 16 , —NR 15 S(O) 2 R 16 , —NR 15 C(O)NR 16 R 17 , substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl;
 R 15 , R 16  and R 17  are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; and 
 R 15  and R 16 , R 16  and R 17  or R 15  and R 17  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring; 
 
 R 1  is selected from the group consisting of —C(O)R 7 , —CO 2 R 7 , —C(O)NR 7 R 8 , —S(O)R 7 , —S(O) 2 R 7 , —S(O) 2 NR 7 R 8 , substituted or unsubstituted C 2 -C 8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl; 
 R 2  is selected from the group consisting of hydrogen, halogen, —CN, —C(O)R 7 , —CO 2 R 7 , —C(O)NR 7 R 8 , —OR 7 , —OC(O)R 7 , —OC(O)NR 7 R 8 , —SR 7 , —S(O)R 7 , —S(O) 2 R 7 , —S(O) 2 NR 7 R 8 , —NO 2 , —NR 7 R 8 , —NR 7 C(O)R 8 , —NR 7 C(O)OR 8 , —NR 7 S(O) 2 R 8 , —NR 7 C(O)NR 8 R 9 , substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl;
 R 7 , R 8 , and R 9  are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8 alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; 
 R 7  and R 8 , R 8  and R 9  or R 7  and R 9  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring; and 
 
 where R 1  and R 2  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring. 
 
     
     
       2. The compound of  claim 1 , or a salt thereof, of the formula (II): 
       
         
           
           
               
               
           
         
       
       where
 X 1 , X 2 , X 3 , X 4 , and X 5  are each independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, —CN, —NO 2 , —C(O)R 18 , —CO 2 R 18 , —C(O)NR 18 R 19 , —OR 18 , —OC(O)R 19 , —OC(O)NR 18 R 19 , —NR 18 C(O)R 19 , —NR 18 C(O)NR 19 R 20 , —NR 18 R 19 , —NR 18 CO 2 R 19 , —NR 18 S(O) 2 R 19 , —SR 18 , —S(O)R 18 , —S(O) 2 R 18 , —S(O) 2 NR 18 R 19 , substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl;
 R 18 , R 19  and R 20  re each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; and 
 R 18  and R 19 , R 19  and R 20  or R 18  and R 20  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring. 
 
 
     
     
       3. The compound of  claim 2 , or a salt thereof, where
 X 1  is selected from the group consisting of halogen, substituted or unsubstituted C 1-8  alkyl, —OR 18 , —NR 18 R 19 , and substituted or unsubstituted 3- to 10-membered heterocyclyl; 
 Y 7  is hydrogen; 
 Y 4 , Y 5 , and Y 6  are each independently selected from the group consisting of hydrogen, halogen, —CN, —CO 2 R 15 —C(O)NR 15 R 16 ; 
 R 1  is selected from the group consisting of substituted or unsubstituted C 2 -C 8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl; and 
 R 2  is selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl. 
 
     
     
       4. The compound of  claim 2 , or a salt thereof, of the formula (III): 
       
         
           
           
               
               
           
         
       
       where at least one of X 1  and X 2  is other than hydrogen and at least one of Y 4  and Y 5  is other than hydrogen. 
     
     
       5. The compound of  claim 4 , or a salt thereof, of the formula (III): 
       where X 2  is hydrogen or halogen; Y 4  is hydrogen, halogen or —CN; and X 1  and Y 5  are other than hydrogen. 
     
     
       6. The compound of  claim 5 , or a salt thereof, where
 X 1  is selected from the group consisting of substituted or unsubstituted C 1-8  alkyl, —OR 18 , —NR 18 R 19 , and substituted or unsubstituted 3- to 10-membered heterocyclyl; 
 Y 5  is selected from the group consisting of halogen, —CN, —CO 2 R 15 , and —C(O)NR 15 R 16 ; 
 R 1  is selected from the group consisting of substituted or unsubstituted C 2 -C 8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl; and 
 R 2  is hydrogen. 
 
     
     
       7. The compound of  claim 6 , or a salt thereof, of the formula (VIII) 
       
         
           
           
               
               
           
         
       
       where W is NH or O; and n is 0, 1, or 2. 
     
     
       8. The compound of  claim 4 , or a salt thereof, where
 X 1  is halogen; 
 X 2  is halogen or —CF 3 ; 
 Y 4  is halogen; 
 Y 5  is hydrogen or halogen; 
 R 2  is hydrogen or substituted or unsubstituted C 1-8  alkyl. 
 
     
     
       9. The compound of  claim 8 , or a salt thereof, of the formula (V): 
       
         
           
           
               
               
           
         
       
     
     
       10. The compound of  claim 2 , or a salt thereof, of the formula (IV): 
       
         
           
           
               
               
           
         
       
       where Y 4  is hydrogen or fluoro; and X 1  and Y 5  are other than hydrogen. 
     
     
       11. The compound of  claim 10 , or a salt thereof, where
 X 1  is selected from the group consisting of substituted or unsubstituted C 1-8  alkyl, —OR 18 , —NR 18 R 19 , and substituted or unsubstituted 3- to 10-membered heterocyclyl; 
 Y 5  is selected from the group consisting of halogen, —CN, —CO 2 R 15 , —C(O)NR 15 R 16    
 R 1  is selected from the group consisting of substituted or unsubstituted C 2 -C 8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl; and 
 R 2  is selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl. 
 
     
     
       12. The compound of  claim 11 , or a salt thereof, of the formula (VI): 
       
         
           
           
               
               
           
         
       
     
     
       13. The compound of  claim 12 , or a salt thereof, of the formula (VII): 
       
         
           
           
               
               
           
         
       
       where
 R 3  and R 4  are each independently hydrogen, unsubstituted or substituted C 1-8  alkyl, or R 3  and R 4  together with the carbon which they substitute form a 3-10 member carbocyclic, 4-10 member heterocyclic, 5-10 member heteroaryl ring or 6-10 membered aryl ring. 
 
     
     
       14. The compound of  claim 13 , or salt thereof, where R 2  is hydrogen. 
     
     
       15. A compound of  claim 1 , selected from the group consisting of:
 4-tert-butyl-N-(4-chloro-2-(4,5-diisopropyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4,5-dimethyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-cyclopentyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-cyclopropyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-ethyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-isopropyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-isopropyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(tetrahydro-2H-pyran-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-phenyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-(methoxymethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-ethyl-4-isopropyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-isopropyl-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(1H-pyrazol-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(pyridin-2-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(tetrahydro-2H-pyran-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-phenyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 N-(4-chloro-2-(4-isopropyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)-4-isopropoxybenzenesulfonamide; 
 N-(2-(3-(2-(4-tert-butylphenylsulfonamido)-5-chlorophenyl)-5-methyl-4H-1,2,4-triazol-4-yl)ethyl)acetamide; 
 (R)-4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(tetrahydrofuran-2-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4,5-difluoro-2-(4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(4-(1-hydroxypropan-2-yl)-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(tetrahydrofuran-2-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(2-(4-ethyl-4H-1,2,4-triazol-3-yl)-4,5-difluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(2-(4-ethyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4,5-difluoro-2-(4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4,5-diethyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4,5-dimethyl-4H-1,2,4-triazol-3-yl)-3-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4,5-dimethyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-ethyl-4H-1,2,4-triazol-3-yl)-3-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-ethyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-ethyl-5-isopropyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-ethyl-5-methyl-4H-1,2,4-triazol-3-yl)-3-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-isobutyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(oxazol-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-((dimethylamino)methyl)-4-methyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-(2-methoxyethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-(methoxymethyl)-4-(tetrahydro-2H -pyran-4-yl)-4H -1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(piperidin-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(piperidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(5-chloro-2-(4-isopropyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(5-chloro-2-(4-isopropyl-5-(4-methyltetrahydro-2H-pyran-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(5-fluoro-2-(4-isopropyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 N-(4-chloro-2-(4-ethyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)-4-isopropoxybenzenesulfonamide; 
 ethyl 2-(5-(2-(4-tert-butylphenylsulfonamido)-5-chloro-4-fluorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl)acetate; 
 5-(2-(4-tert-butylphenylsulfonamido)-5-chloro-4-fluorophenyl)-4-methyl-4H-1,2,4-triazole-3-carboxamide; 
 5-(2-(4-tert-butylphenylsulfonamido)-5-chloro-4-fluorophenyl)-N,4-dimethyl-4H-1,2,4-triazole-3-carboxamide; 
 (R)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(1-hydroxyethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(4-(piperidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(4-(tetrahydro-2H-pyran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(piperidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(piperidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(1-hydroxyethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-methyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)—N-(4-chloro-2-(4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)-4-isopropoxybenzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-isopropyl-5-(tetrahydro-2H-pyran-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(5-methyloxazol-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-((cyclopropylamino)methyl)-4-methyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-((ethylamino)methyl)-4-methyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-ethyl-4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-ethyl-4-methyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-ethyl-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(tetrahydro-2H-pyran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-isopropyl-5-(methoxymethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-((methylamino)methyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(methylsulfonylmethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(morpholinomethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(oxazol-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(pyrrolidin-1-ylmethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(tetrahydro-2H-pyran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(tetrahydro-2H-pyran-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-((isopropylamino)methyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(1-hydroxyethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(2-hydroxy-2-methylpropyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(2-hydroxypropan-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(2-methoxyethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(hydroxymethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(methoxymethyl)-4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(methoxymethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 N-(2-(5-(azetidin-1-ylmethyl)-4-methyl-4H-1,2,4-triazol-3-yl)-4-chloro-5-fluorophenyl)-4-tert-butylbenzenesulfonamide; 
 N-(2-(5-acetyl-4-methyl-4H-1,2,4-triazol-3-yl)-4-chloro-5-fluorophenyl)-4-tert-butylbenzenesulfonamide; 
 (S)-4-tert-butyl-N-(4,5-difluoro-2-(5-methyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(5-ethyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(5-isopropyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(2-(4,5-dimethyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(2-(4-ethyl-5-methyl-4H-1,2,4-triazol-3-yl)-4,5-difluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(2-(4-ethyl-5-methyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(piperidin-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-isopropyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-isopropyl-5-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(5-methyloxazol-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-isopropyl-4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-methyl-4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 N-(4-chloro-2-(4,5-dimethyl-4H-1,2,4-triazol-3-yl)phenyl)-4-isopropoxybenzenesulfonamide; 
 N-(4-chloro-2-(4-isopropyl-4H-1,2,4-triazol-3-yl)phenyl)-4-isopropoxybenzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(5-ethyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(2-oxopyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-isopropyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)—N-(4-chloro-2-(4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)-4-(4-methyltetrahydro-2H-pyran-4-yl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-cyclobutyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-ethyl-5-isopropyl-4H-1,2,4-triazol-3-yl)-5-fluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-isopropyl-5-(trifluoromethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(1-methylpiperidin-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(2-(methylsulfonyl)ethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 N-(2-(4-(1-acetylpiperidin-4-yl)-5-methyl-4H-1,2,4-triazol-3-yl)-4-chlorophenyl)-4-tert-butylbenzenesulfonamide; 
 N-(2-(4-(2-aminoethyl)-5-methyl-4H-1,2,4-triazol-3-yl)-4-chlorophenyl)-4-tert-butylbenzenesulfonamide; 
 N-(2-(4-(azetidin-3-yl)-4H-1,2,4-triazol-3-yl)-4-chloro-5-fluorophenyl)-4-tert-butylbenzenesulfonamide; 
 (R)-4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(2-(4,5-dimethyl-4H-1,2,4-triazol-3-yl)-4,5-difluorophenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-isopropyl-5-(methoxymethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(pyridin-2-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(tetrahydrofuran-2-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-((dimethylamino)methyl)-4-isopropyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-(isopropoxymethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-(3-(2-(4-tert-butylphenylsulfonamido)-5-chlorophenyl)-5-methyl-4H-1,2,4-triazol-4-yl)piperidine-1-carboxamide; 
 4-tert-butyl-N-(4-chloro-2-(4-(2-(dimethylamino)ethyl)-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(1-(methylsulfonyl)piperidin-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-methyl-4-(2-(methylamino)ethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(5-chloro-2-(4-isopropyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 N-(2-(4-(1-acetylpyrrolidin-3-yl)-5-methyl-4H-1,2,4-triazol-3-yl)-4-chlorophenyl)-4-tert-butylbenzenesulfonamide; 
 N-(2-(5-amino-4-isopropyl-4H-1,2,4-triazol-3-yl)-4-chlorophenyl)-4-tert-butylbenzenesulfonamide; 
 (R)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(tetrahydrofuran-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (R)-4-tert-butyl-N-(4-chloro-2-(4-(pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-cyano-2-(5-ethyl-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-(4-tert-butylphenylsulfonamido)-3-(5-ethyl-4-methyl-4H-1,2,4-triazol-3-yl)benzamide; 
 4-(4-tert-butylphenylsulfonamido)-3-(5-ethyl-4-methyl-4H-1,2,4-triazol-3-yl)benzoic acid; 
 N-(2-(4-(azetidin-3-yl)-4H-1,2,4-triazol-3-yl)-4-chlorophenyl)-4-tert-butylbenzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-5-((methylamino)methyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 methyl 4-(4-tert-butylphenylsulfonamido)-3-(5-ethyl-4-methyl-4H-1,2,4-triazol-3-yl)benzoate; 
 N-(4-chloro-2-(4,5-dimethyl-4H-1,2,4-triazol-3-yl)phenyl)-3-fluoro-4-morpholinobenzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-(2-methoxyethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(2-hydroxyethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(5-((isopropylamino)methyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(1-methoxyethyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (R)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(pyrrolidin-2-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(4-(1-isopropylpyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-3-(3-(2-(4-tert-butylphenylsulfonamido)-5-chlorophenyl)-4H-1,2,4-triazol-4-yl)pyrrolidine-1-carboxamide; 
 4-tert-butyl-N-(4-chloro-2-(4-methyl-5-(morpholinomethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(piperidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-(piperazin-1-ylmethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-((tetrahydrofuran-3-ylamino)methyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(5-(((2-methoxyethyl)(methyl)amino)methyl)-4-methyl-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-2-(4-isopropyl-5-(4-methyltetrahydro-2H-pyran-4-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-((4-methylpiperazin-1-yl)methyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-methyl-5-((tetrahydro-2H-pyran-4-ylamino)methyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 (S)-4-tert-butyl-N-(4-chloro-2-(4-(1-(methylsulfonyl)pyrrolidin-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 4-tert-butyl-N-(4-chloro-5-fluoro-2-(4-isopropyl-5-(morpholinomethyl)-4H-1,2,4-triazol-3-yl)phenyl)benzenesulfonamide; 
 N-(2-(4-(1H-pyrazol-3-yl)-4H-1,2,4-triazol-3-yl)-5-chlorophenyl)-4-chloro-3-(trifluoromethyl)benzenesulfonamide; 
 4-chloro-N-(5-chloro-2-(5-methyl-4-(1H-pyrazol-3-yl)-4H-1,2,4-triazol-3-yl)phenyl)-3-(trifluoromethyl)benzenesulfonamide; 
 4-chloro-N-(5-chloro-2-(4-phenyl-4H-1,2,4-triazol-3-yl)phenyl)-3-(trifluoromethyl)benzenesulfonamide; 
 N-(2-(4-(1H-pyrazol-3-yl)-4H-1,2,4-triazol-3-yl)-5-chloro-4-fluorophenyl)-4-chloro-3-(trifluoromethyl)benzenesulfonamide; 
 5-(4-chloro-2-(4-chloro-3-(trifluoromethyl)phenylsulfonamido)-5-fluorophenyl)-4-(1H-pyrazol-3-yl)-4H-1,2,4-triazole-3-carboxamide; and 
 N-(2-([1,2,4]triazolo[4,3-a]pyrimidin-3-yl)-4-chlorophenyl)-4-tert-butylbenzenesulfonamide. 
 
     
     
       16. A composition comprising a pharmaceutically acceptable carrier and a compound of  claim 1 . 
     
     
       17. A compound of  claim 1 , wherein R 1  is selected from the group consisting of: —C(O)R 7 , —CO 2 R 7 , —C(O)NR 7 R 8 , —S(O)R 7 , —S(O) 2 R 7 , —S(O) 2 NR 7 R 8 , substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl. 
     
     
       18. A compound of the formula (II), or a salt thereof: 
       
         
           
           
               
               
           
         
         where X 1  is selected from the group consisting of halogen, substituted or unsubstituted C 1-8  alkyl, —OR 18 , —NR 18 R 19 , and substituted or unsubstituted 3- to 10-membered heterocyclyl; 
         X 2 , X 3 , X 4 , and X 5  are each independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 1-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, —CN, —NO 2 , 
         —C(O)R 18 , —CO 2 R 18 , —C(O)NR 18 R 19 , —OR 18 , —OC(O)R 19 , —OC(O)NR 18 R 19 , —NO 2 , —NR 18 C(O)R 19 , —NR 18 C(O)NR 19 R 20 , —NR 18 R 19 , —NR 18 CO 2 R 19 , —NR 18 S(O) 2 R 19 , —SR 18 , —S(O)R 18 , —S(O) 2 R 18 , —S(O) 2 NR 18 R 19 , substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; 
         R 18 , R 19  and R 20  are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; and 
         R 18  and R 19 , R 19  and R 20  or R 18  and R 20  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring; 
         Y 4 , Y 5 , and Y 6  are each independently selected from the group consisting of hydrogen, halogen, —ON, —CO 2 R 15 , —C(O)NR 15 R 16 ; 
         R 15  and R 16  are each independently selected from the group consisting of: hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; and 
         R 15  and R 16  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring; 
         Y 7  is hydrogen; 
         R 1  is selected from the group consisting of substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl; and 
         R 2  is selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl. 
       
     
     
       19. A compound or a salt thereof, of the formula (III): 
       
         
           
           
               
               
           
         
         X 1  is selected from the group consisting of substituted or unsubstituted C 1-8  alkyl, —OR 18 , —NR 18 R 19 , and substituted or unsubstituted 3- to 10-membered heterocyclyl;
 R 18  and R 19  are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; 
 R 18  and R 19  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring; 
 
         X 2  is hydrogen or halogen; 
         Y 4  is hydrogen, halogen, or —CN; 
         Y 5  is selected from the group consisting of halogen, —CN, —CO 2 R 15 , and —C(O)NR 15 R 16 ;
 R 15  and R 16  are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; and 
 R 15  and R 16  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring; 
 
         R 1  is selected from the group consisting of substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl; 
         R 2  is hydrogen. 
       
     
     
       20. A compound or a salt thereof, of the formula (IV): 
       
         
           
           
               
               
           
         
         where X 1  is selected from the group consisting of substituted or unsubstituted C 1-8  alkyl, —OR 18 , —NR 18 R 19 , and substituted or unsubstituted 3- to 10-membered heterocyclyl;
 R 18  and R 19  are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; 
 R 18  and R 19  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring; 
 
         Y 4  is hydrogen or fluoro; 
         Y 5  is selected from the group consisting of halogen, —CN, —CO 2 R 15 , —C(O)NR 15 R 16 ;
 R 15  and R 16  are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted C 2-8  alkenyl, substituted or unsubstituted C 2-8  alkynyl, substituted or unsubstituted C 6-10  aryl, substituted or unsubstituted 5- to 10-membered heteroaryl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; and 
 R 15  and R 16  may, together with the atoms to which they are attached, form a substituted or unsubstituted 5-, 6-, or 7-membered ring; 
 
         R 1  is selected from the group consisting of substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl; and 
         R 2  is selected from the group consisting of hydrogen, substituted or unsubstituted C 1-8  alkyl, substituted or unsubstituted 3- to 10-membered heterocyclyl, substituted or unsubstituted C 6-10  aryl, and substituted or unsubstituted 5- to 10-membered heteroaryl. 
       
     
     
       21. The compound of  claim 20 , or a salt thereof, of the formula (VI): 
       
         
           
           
               
               
           
         
       
     
     
       22. The compound of  claim 21 , or a salt thereof, of the formula (VII): 
       
         
           
           
               
               
           
         
       
       where R 3  and R 4  are each independently hydrogen, unsubstituted or substituted C 1-8  alkyl, or R 3  and R 4  together with the carbon which they substitute form a 3-10 member carbocyclic, 4-10 member heterocyclic, 5-10 member heteroaryl ring or 6-10 membered aryl ring. 
     
     
       23. The compound of  claim 22 , or salt thereof, where R 2  is hydrogen.
Cited by (0)

No later patents cite this yet.
References (0)

No backward citations on record.